telapristone

Telapristone is a synthetic, steroidal selective progesterone receptor modulator (SPRM) related to mifepristone. It acts as a selective antagonist of the progesterone receptor and has been developed primarily for the treatment of uterine fibroids and endometriosis. Telapristone competitively binds to the progesterone receptor in target tissues, inhibiting PR-mediated gene expression and thus interfering with progesterone activity in the reproductive system. This results in suppression of ovulation and inhibition of endometrial tissue proliferation. Additionally, it may have antineoplastic effects by inducing apoptosis in estrogen receptor (ER) and PR-positive breast cancer cells through downregulation of ER and suppression of cyclin-dependent kinases CDK2/4, leading to G1/S cell cycle arrest. Unlike some other SPRMs, telapristone does not exhibit estrogenic or androgenic activities but does have some antiglucocorticoid activity[1][3][6].

Brand names

ProellexProgenta

Other names

telapristone acetate